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Cat. No.: HY-184293

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PROTAC ATR degrader-4

PROTAC ATR degrader-4 is a PROTAC-based ATR kinase degrader, with a DC₅₀ of 6.18 μM and a D_max of 71.42% in LoVo cells. PROTAC ATR degrader-4 downregulates ATR protein expression, inducing nuclear envelope rupture, genomic instability, DNA damage and apoptosis. PROTAC ATR degrader-4 exhibits anti-tumor activity in xenograft tumor mouse models and can be used for the research of atm-deficient cancers.
(Pink: ATM/ATR ligand (HY-184294 ); Blue: Cereblon ligand (HY-10984); Black: linker).

For research use only. We do not sell to patients.

Formula: C₃₅H₃₄N₈O₆
Molecular Weight:662.69

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC ATR degrader-4 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC ATR degrader-4 is a PROTAC-based ATR kinase degrader, with a DC₅₀ of 6.18 μM and a D_max of 71.42% in LoVo cells. PROTAC ATR degrader-4 downregulates ATR protein expression, inducing nuclear envelope rupture, genomic instability, DNA damage and apoptosis. PROTAC ATR degrader-4 exhibits anti-tumor activity in xenograft tumor mouse models and can be used for the research of atm-deficient cancers^[1]. (Pink: ATM/ATR ligand (HY-184294 ); Blue: Cereblon ligand (HY-10984); Black: linker).

All PROTACs Isoforms :

All ATM/ATR Isoforms :

In Vitro

OthersAnti-cancerCytokines and ChemokinesApoptosisCell Cycle Regulation

Others

PROTAC ATR degrader-4 (compound I-1) (100 nM) binds to ATR kinase and inhibits its activity by 60.2% at a concentration of 100 nM^[1].

Anti-cancer

PROTAC ATR degrader-4 (72 h) exhibits potent antiproliferative activity in ATM-deficient cancer cells (LoVo, NCI-H23, GRANTA-519) and ATM-proficient HCT116 cells, with minimal cytotoxicity in normal NCM460 cells, achieving an IC₅₀ of 4.5 μM in LoVo cells^[1].

Others

PROTAC ATR degrader-4 (1.56-25 μM; 48 h) selectively degrades ATR protein in LoVo and HCT116 cells, with no observable degradation of other PIKK family members, DDR-related proteins, or GSPT1 at concentrations up to 25 μM^[1].

Others

PROTAC ATR degrader-4 (6.25 μM; 48 h)-mediated ATR protein degradation in LoVo cells is dependent on ATR binding, CRBN recruitment, the ubiquitination system, and the proteasomal degradation pathway^[1].

Cytokines and Chemokines

PROTAC ATR degrader-4 (1.56-25 μM; 48 h) inhibits the ATR/CHK1 signaling pathway in LoVo cells by reducing ATR protein levels and subsequent phosphorylation of ATR and CHK1, without degrading CHK1 itself^[1].

Apoptosis

PROTAC ATR degrader-4 (5-10 μM; 72 h) induces dose-dependent DNA damage in LoVo cells, with more significant effects than the ATR inhibitor ZH-25 at lower concentrations^[1].

Apoptosis

PROTAC ATR degrader-4 (5-10 μM; 48 h) induces dose-dependent apoptosis in LoVo cells, with greater activity at 5 μM than the ATR inhibitor ZH-25 at 10 μM^[1].

Cell Cycle Regulation

PROTAC ATR degrader-4 (5-10 μM; 48 h) reduces the G2/M phase population in LoVo cells at 5 μM similar to the ATR inhibitor ZH-25, but has minimal cell cycle effects at 10 μM, suggesting potential kinase-independent antitumor mechanisms^[1].

Anti-cancer

PROTAC ATR degrader-4 (5-25 μM; 24 h) disrupts nuclear envelope integrity in LoVo cells, leading to increased DNA damage and apoptosis markers in a concentration-dependent manner, with more potent effects than the ATR inhibitor ZH-25, indicating kinase-independent antitumor activity^[1].

Others

PROTAC ATR degrader-4 (3.13-25 μM; 48 h) exerts its effects in LoVo cells by degrading ATR protein rather than inhibiting ATR transcription^[1].

Anti-cancer

PROTAC ATR degrader-4 (48 h) exhibits synergistic antiproliferative activity with the ATM inhibitor AZ32 in ATM-proficient HCT116 cells, reducing its IC₅₀ from 15.57 μM to 7.89 μM when combined with 2 μM AZ32^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-t	V_ss	CL
Rat^[1]	1 mg/kg	i.v.	2.54 h	3944.78 ng/mL	2267.80	4607 L/kg	0.44 L/h/kg

In Vivo

Anti-cancer

PROTAC ATR degrader-4 (compound I-1) (25-50 mg/kg; i.p.; daily; 14 days) exhibits significant dose-dependent anti-tumor activity in BALB/c nude mice bearing LoVo xenografts, reducing ATR protein levels by up to ~75% at the 50 mg/kg dose with good safety^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft model)^[1]
Dosage:

25 mg/kg; 50 mg/kg
Administration:

i.p.; daily; 14 days
Result:

Inhibited LoVo xenograft tumor growth in a dose-dependent manner.
Reduced ATR protein levels in tumor tissue to ~65% of the control group at 25 mg/kg.
Reduced ATR protein levels in tumor tissue to ~25% of the control group at 50 mg/kg.
Caused no significant changes in mouse body weight during the treatment period.

Related Protocols :

Chemical Information

Molecular Weight 662.69
Formula C₃₅H₃₄N₈O₆
SMILES

C[C@@H]1COCCN1C2=NC(C3=CC=CC4=C3C=CN4)=NC5=C2CCN(C5)CC(NC6=C7C(N(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Huang L, et al.. Discovery of a selective and effective CRBN-recruiting ATR degrader with strong antitumor activity. European journal of medicinal chemistry. 2026 Oct 05;315:118976. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC ATR degrader-4

All PROTACs Isoforms

All ATM/ATR Isoforms

Biological Activity

Description

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC ATR degrader-4 Related Classifications

HY-184293 Related Classifications

Bioz

Keywords

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